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Application of flufenamic acid as effective component in preparation of airway smooth muscle relaxation agent

A technology of airway smooth muscle and flufenamic acid, which is applied in the field of application of flufenamic acid as an active ingredient in the preparation of airway smooth muscle relaxants, can solve the problems of lack of powerful TAS2R agonists, and achieve broad application prospects Effect

Pending Publication Date: 2021-11-26
CHANGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But so far, there is still a lack of potent TAS2R agonists that can be used as new pharmaceutical agents for patients with severe asthma

Method used

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  • Application of flufenamic acid as effective component in preparation of airway smooth muscle relaxation agent
  • Application of flufenamic acid as effective component in preparation of airway smooth muscle relaxation agent
  • Application of flufenamic acid as effective component in preparation of airway smooth muscle relaxation agent

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] (1) Experimental object

[0043] Primary culture of human ASMCs

[0044] (2) Experimental equipment

[0045] Optical magnetic particle torsion cell analysis system (OMTC), live cell workstation, detachable 96-well plate, ultra-clean workbench, CO 2 Cell incubator, low-speed centrifuge, cell counting plate, constant temperature water bath, autoclave, confocal culture dish.

[0046] (3) Experimental process

[0047] From the BitterDB database, 16 bitter substances (flufenamic acid, kaempferol, 1,10-phenanthroline, carlipidol, andrographolide, benzodinaridine) that can activate bitter taste receptors at concentrations below 10 μM were screened out. ammonium, hesperetin, quinine, chloroquine, naringenin, benzoin, tangeretin, apigenin, quercetin, cucurbitacin E, artesunate). After the cells were treated with the above 16 different bitter substances, the change of cell stiffness was detected by optical magnetic particle torsion cytometry, so as to evaluate the relaxation ...

Embodiment 2

[0056] (1) Experimental object

[0057] Primary culture of human ASMCs

[0058] (2) Experimental equipment

[0059] Optical magnetic particle torsion cell analysis system (OMTC), live cell workstation, detachable 96-well plate, ultra-clean workbench, CO 2 Cell incubator, low-speed centrifuge, cell counting plate, constant temperature water bath, autoclave, confocal culture dish.

[0060] (3) Experimental process

[0061] ASMCs were treated with flufenamic acid after inhibiting bitter taste receptors and downstream signaling pathways, and changes in cell stiffness were detected by optical magnetic particle torsion cytometry. The specific method is to inoculate the cells in a detachable 96-well plate at a seeding density of 1×10 4 After 24 hours of adherent growth, the IT medium was replaced for 12 hours, and the ASMCs were treated with siRNA targeting TAS2R14 for 48 hours to reduce the expression of bitter taste receptor 14, U73122 (20 μmol / L) to inhibit the activity of pho...

Embodiment 3

[0068] (1) Experimental object

[0069] BALB / c mouse

[0070] (2) Experimental equipment

[0071] FlexiVent small animal lung function measuring instrument, ultra-clean workbench, constant temperature water bath.

[0072] (3) Experimental process

[0073] The airway resistance of normal and asthma model mice was detected by FlexiVent small animal pulmonary function measuring instrument, and the airway diastolic function of flufenamic acid was evaluated. First, the animals were randomly divided into 6 groups: normal control group, asthma model group (ovalbumin treatment) control group, flufenamic acid high, medium and low dose groups (8mg / kg, 4mg / kg, 2mg / kg) And albuterol group (8mg / kg), 5 rats in each group.

[0074] The process of establishing the asthma model was to inject 200 μL ovalbumin sensitizer into each mouse intraperitoneally on the 1st and 7th day, and give 100 μL ovalbumin sensitizer to the intraperitoneal injection on the 14th day; the normal control group was...

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Abstract

The invention discloses an application of flufenamic acid as an effective component in preparation of an airway smooth muscle relaxation agent. Experiments reveal for the first time that a compound (CID: 3371) can activate bitter taste receptors and strongly relax airway smooth muscle cells, and the relaxation degree of the compound is close to that of isoproterenol and salbutamol; and it is prompted that the compound (CID: 3371) can be used for preparing an airway smooth muscle relaxation medicine and also can be used for preparing the airway smooth muscle relaxation agent, so that the compound is used for asthma, chronic obstructive pulmonary diseases and the like, and has a wide application prospect.

Description

technical field [0001] The invention belongs to the technical field, and in particular relates to the application of flufenamic acid as an active ingredient in the preparation of an airway smooth muscle relaxant. Background technique [0002] Asthma is a common chronic respiratory disease. There are as many as 300 million asthma patients worldwide. Although the pharmaceutical industry has made great progress, it still brings a large economic burden to the society. There are nearly 50 million asthma patients in China, and its prevalence is increasing year by year. The burden of asthma has risen by 20% over the past 20 years, although advances in science and technology have led to declines in hospitalization and mortality in some regions. [0003] Asthma is characterized by symptoms such as recurrent wheezing, chest tightness, pulmonary obstruction, and respiratory insufficiency, and these respiratory symptoms are mainly caused by airway obstruction. Airway smooth muscle cel...

Claims

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Application Information

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IPC IPC(8): A61K31/196A61P11/08A61P11/06
CPCA61K31/196A61P11/08A61P11/06
Inventor 罗明志倪凯田姈玉郭佳刘磊李晶晶潘艳邓林红
Owner CHANGZHOU UNIV
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